Synthesis, antimalarial and antitubercular activity of acetylenic chalcones

Renate H Hans; Eric M Guantai; Carmen Lategan; Peter J Smith; Baojie Wan; Scott G Franzblau; Jiri Gut; Philip J Rosenthal; Kelly Chibale

doi:10.1016/j.bmcl.2009.12.062

Synthesis, antimalarial and antitubercular activity of acetylenic chalcones

Bioorg Med Chem Lett. 2010 Feb 1;20(3):942-4. doi: 10.1016/j.bmcl.2009.12.062. Epub 2009 Dec 23.

Authors

Renate H Hans¹, Eric M Guantai, Carmen Lategan, Peter J Smith, Baojie Wan, Scott G Franzblau, Jiri Gut, Philip J Rosenthal, Kelly Chibale

Affiliation

¹ Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.

PMID: 20045640
DOI: 10.1016/j.bmcl.2009.12.062

Abstract

A series of acetylenic chalcones were evaluated for antimalarial and antitubercular activity. The antimalarial data for this series suggests that growth inhibition of the W2 strain of Plasmodium falciparum can be imparted by the introduction of a methoxy group ortho to the acetylenic group. Most compounds were more active against non-replicating than replicating cultures of Mycobacterium tuberculosis H(37)Rv, an unusual pattern with respect to existing anti-TB agents.

Publication types

Comparative Study
Research Support, Non-U.S. Gov't

MeSH terms

Alkynes / chemical synthesis*
Alkynes / pharmacology
Antimalarials / chemical synthesis*
Antimalarials / pharmacology
Antitubercular Agents / chemical synthesis*
Antitubercular Agents / pharmacology
Chalcones / chemical synthesis*
Chalcones / pharmacology
Mycobacterium tuberculosis / drug effects
Mycobacterium tuberculosis / physiology
Plasmodium falciparum / drug effects
Plasmodium falciparum / physiology

Substances

Alkynes
Antimalarials
Antitubercular Agents
Chalcones